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Cat. No.: HY-146807

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Type II TRK inhibitor 1

Type II TRK inhibitor 1 is a potent TRK inhibitor, which inhibits various TRK fusion protein variants and wild type. Type II TRK inhibitor 1 exhibits antiproliferative activity against Ba/F3 cells harboring CD74-TRKA^G667C and ETV6-TRKC^G696C fusion proteins with IC₅₀s of 6 nM and 1.7 nM, respectively. Type II TRK inhibitor 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

For research use only. We do not sell to patients.

CAS No.: 2937543-72-9
Formula: C₃₅H₃₃F₃N₈O₃
Molecular Weight:670.68

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (272 KB)

Type II TRK inhibitor 1 Chemical Structure

CAS No.: 2937543-72-9

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Type II TRK inhibitor 1 is a potent TRK inhibitor, which inhibits various TRK fusion protein variants and wild type. Type II TRK inhibitor 1 exhibits antiproliferative activity against Ba/F3 cells harboring CD74-TRKA^G667C and ETV6-TRKC^G696C fusion proteins with IC₅₀s of 6 nM and 1.7 nM, respectively^[1]. Type II TRK inhibitor 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC₅₀ & Target^[1]

TrkA

TrkC

All Trk Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	0.006 μM Compound: 7b	Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G667C mutant assessed as cell growth inhibition incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G667C mutant assessed as cell growth inhibition incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	0.023 μM Compound: 7b	Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC assessed as cell growth inhibition incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC assessed as cell growth inhibition incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	0.034 μM Compound: 7b	Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA assessed as cell growth inhibition incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA assessed as cell growth inhibition incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	0.11 μM Compound: 7b	Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G595R mutant assessed as cell growth inhibition incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G595R mutant assessed as cell growth inhibition incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	1.7 nM Compound: 7b	Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G696C mutant incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G696C mutant incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	13.4 nM Compound: 7b	Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G696S mutant incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G696S mutant incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	16.3 nM Compound: 7b	Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC V573M mutant incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC V573M mutant incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	3.2 nM Compound: 7b	Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G696A mutant incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G696A mutant incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	3.8 nM Compound: 7b	Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G667A mutant incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G667A mutant incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	30.8 nM Compound: 7b	Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G667S mutant incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA G667S mutant incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	5.6 nM Compound: 7b	Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G623E mutant incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G623E mutant incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	55 nM Compound: 7b	Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G623R mutant incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing ETV6 fused TRKC G623R mutant incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	>10000 nM Compound: 7b	Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell growth incubated for 3 days by CCK8 assay Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell growth incubated for 3 days by CCK8 assay	[PMID: 35426680]
BaF3	IC₅₀	113.6 nM Compound: 8	Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G595R mutant fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G595R mutant fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	23.66 nM Compound: 8	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-NTRK3 fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-NTRK3 fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	33.59 nM Compound: 8	Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	6.02 nM Compound: 8	Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G667C mutant fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G667C mutant fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]

In Vitro

Type II TRK inhibitor 1 (compound 7b) (3.1-800 nM; 2 h) inhibits the phosphorylation of TRKA, PLCγ1, and ERK^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

Ba/F3 engineered cells harboring CD74-TRKA, CD74-TRKA^G667C, and CD74-TRKA^G595R
Concentration:

0 nM, 3.1 nM, 12.5 nM, 50 nM, 200 nM, 800 nM
Incubation Time:

24 hours
Result:

Decreased the protein level of p-TRKA, p-PLCγ1, p-ERK in cells.

Chemical Information

CAS No. 2937543-72-9
Molecular Weight 670.68
Formula C₃₅H₃₃F₃N₈O₃
SMILES

CN(CCN1)C2=NN3C(C=C2)=NC=C3C#CC4=CC(OCCCCC1=O)=CC(C(NC5=CC(N6C=C(C)N=C6)=CC(C(F)(F)F)=C5)=O)=C4C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Wang Z, et al. Discovery of the First Highly Selective and Broadly Effective Macrocycle-Based Type II TRK Inhibitors that Overcome Clinically Acquired Resistance. J Med Chem. 2022 Apr 28;65(8):6325-6337. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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Type II TRK inhibitor 1

All Trk Receptor Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

Type II TRK inhibitor 1 Related Classifications

HY-146807 Related Classifications